Lipid Lowering Drugs (Antilipemic Drugs) (53) Flashcards

1
Q

What are the two primary forms of lipids in the blood

A

Triglycerides and cholesterol

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2
Q

Triglycerides and cholesterol are __ soluble __’s that must be packaged for transport in blood

A

Water soluble fats

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3
Q

____ are the combination of lipids with protein

A

Lipoproteins

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4
Q

Lipoproteins

A

Lipids + proteins

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5
Q

lipids

A

Cholesterol, TGs, others

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6
Q

Proteins

A

On the surface of the particle

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7
Q

Chylomicrons are from

A

The GI tract

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8
Q

Very low density lipoprotein

A

Produced by liver and transports TGs to cells

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9
Q

Low density lipoprotein

A

Less desired, bad cholesterol
-cholesterol rich
-cell membranes and steroid hormones

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10
Q

High density lipoprotein

A

Highly desired
-responsible for recycling of cholesterol
-also known as good cholesterol

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11
Q

Non modifiable factors of coronary artery disease

A

Age, family history, strong history of premature CAD

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12
Q

Age risk factors of CAD: male/female

A

Male- 45+

Female- 55+

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13
Q

Modifiable factors of CAD

A

-current cigarette smoker
-abdominal obesity
-hypertension
-DM
-LDL:HDL ratio

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14
Q

Four groups of lipid lowering drugs

A

-HMG CoA reductase inhibitors
-inhibitors of cholesterol absorption
-niacin
-fibric acid derivatives

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15
Q

HMG-CoA

A

3-hydroxy-3-methylglutaryl coenzyme A
-one of metabolites in cholesterol synthesis pathway

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16
Q

HMG-CoA reductase

A

Critical enzyme for liver cholesterol production

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17
Q

HMG-CoA reductase inhibitors reduce..

A

Plasma LDL levels

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18
Q

Example of HMG-CoA reductase inhibtors

A

Atorvastatin
-end in statin!!!

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19
Q

HMG-CoA reductase inhibtors MOA

A

Inhibit HMG-CoA reductase
-which is an important liver enzyme that produces cholesterol

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20
Q

HMG-CoA reductase inhibtors lower the rate of

A

Cholesterol production
-inc liver LDL receptors
-inc plasma clearance of LDL

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21
Q

Added benefits of statins

A

-decrease VLDL (carry TGs)
-raise HDL (improve LDL/HDL)

22
Q

HMG-CoA reductase inhibtors indications

A

-first line drug therapy for hyper cholesterol Emma
-treatment of types IIa and IIb hyperlipidemias (high LDL) levels

23
Q

HMG-CoA reductase inhibtors adverse effects

A

-GI disturbances
-headache
-muscle pain (myalgia)
-liver injury (raised enzymes)

24
Q

Contraindications of HMG-CoA reductase inhibtors

A

Not used during pregnancy

25
Q

Grapefruit and grapefruit juice

A

Inhibit CYP3A4

26
Q

Three examples of drug inhibitors of CYP3A4

A

-warfarin
-erythromycin
-ritonavir

27
Q

(2) drugs that inhibit cholesterol absorption

A

-bile acid binding resins
-ezetimibe

28
Q

(2) examples of bile acid binding resins

A

Cholestyramine, colestipol

29
Q

When are Cholestyramine, Colestipol taken?

A

Taken before meals
(Bile acid binding resins)

30
Q

Ezetimibe

A

Inhibits cholesterol absorption

31
Q

MOA of bile acid sequestration

A

Prevent reabsorption of bile acids from small intestine

32
Q

Where are bile acids synthesized

A

Synthesized from cholesterol in liver

33
Q

What is the liver stimulated to do?

A

Produce more bile acids

34
Q

Indications of bile acid sequestrants

A

-type II hyperlipoproteinemia
-relief of pruritus associated with partial biliary obstruction

35
Q

Cholestyramine specific Indications

A

Relief of pruritus

36
Q

AE of bile acid sequestrants

A

-GI (constipation, heartburn, nausea, belching, bloating)
-decrease absorption of fat soluble vitamins (A,D,E,K)

37
Q

Examples of fat soluble vitamins (4)

A

A, D, E, K

38
Q

AE of bile acid sequestrants tend to what..

A

Disappear over time

39
Q

fibric acid derivatives MOA (2)

A

Believed*
-activate lipoproteins lipase
-breaks down TGs in lipoproteins
-reduce plasma TGs

Also

-inc fatty acid use in tissues

40
Q

fibric acid derivatives decrease….

A

Plasma triglyceride levels

41
Q

fibric acid derivatives increase…

A

HDL by as much as 10-25%

42
Q

(3) examples of fibric acid derivatives

A

-gemfibrozil
-bezafibrate
-fenofibrate

43
Q

fibric acid derivatives AE

A

-GI (discomfort, diarrhea, nausea)
-blurred vision
-risk of gallstones
-prolonged prothrombin time

44
Q

AE fibric acid derivatives: prolonged prothrombin time

A

-fibrinogen production is reduced
-displacement of anticoagulants from albumin

45
Q

Nicotinic acid or Niacin =

A

Vitamin B3

46
Q

Niacin MOA

A

Reduces plasma TGs

47
Q

Niacin properties

A

-lipid lowering properties

48
Q

Niacin as a vitamin

A

Requires much higher doses (grams) for lipid lowering properties

49
Q

Pro: Niacin

A

Effective, inexpensive, often used in combination with other lipid lowering agents (statins)

50
Q

MOA nicotinic acid

A

Reduces VLDL (carries TGs) from liver
-inhibit lipase = breakdown of lipids
-less fatty acid for TG production in liver

51
Q

AE nicotinic acid

A

-flushing
-pruritus
-GI distress

52
Q

Why does Nicotinic Acid cause flushing, and can it be prevented

A

Due to PG release
-prevent by taking aspirin 30 min before